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Dimebon
Latrepirdine (INN, also known as dimebolin and sold as Dimebon) is an antihistamine drug which has been used clinically in Russia since 1983. Research was conducted in both Russia and western nations into potential applications as a neuroprotective drug to treat Alzheimer's disease and, possibly, as a nootropic, as well. After a major phase III clinical trial for Alzheimer's disease (AD) treatment failed to show any benefit, three other AD trials continued.Novel Alzheimer's Drug Flops ''MedPage Today'', March 03, 2010 Major industry-based development in this indication essentially stopped after another Phase III trial suffered the same fate in 2012.Sweetlove M: Phase III CONCERT Trial of Latrepirdine. Negative results. Pharm Med 2012;26(2):113-115 Latrepirdine failed ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT6 Receptor
The 5HT6 receptor is a subtype of 5HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5HT). It is a G protein-coupled receptor (GPCR) that is coupled to Gs and mediates excitatory neurotransmission. ''HTR6'' denotes the human gene encoding for the receptor. Distribution The 5HT6 receptor is expressed almost exclusively in the brain. It is distributed in various areas including, but not limited to, the olfactory tubercle, cerebral cortex (frontal and entorhinal regions), nucleus accumbens, striatum, caudate nucleus, hippocampus, and the molecular layer of the cerebellum. Based on its abundance in extrapyramidal, limbic, and cortical regions it can be suggested that the 5HT6 receptor plays a role in functions like motor control, emotionality, cognition, and memory. Function Blockade of central 5HT6 receptors has been shown to increase glutamatergic and cholinergic neurotransmission in various brain areas, whereas activation enhances GA ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT5A Receptor
5-Hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein that in humans is encoded by the ''HTR5A'' gene. Agonists and antagonists for 5-HT receptors, as well as serotonin uptake inhibitors, present promnesic (memory-promoting) and/or anti-amnesic effects under different conditions, and 5-HT receptors are also associated with neural changes. Function The gene described in this record is a member of 5-hydroxytryptamine receptor family and encodes a multi-pass membrane protein that functions as a receptor for 5-hydroxytryptamine and couples to G proteins, negatively influencing cAMP levels via Gi and Go. This protein has been shown to function in part through the regulation of intracellular Ca2+ mobilization. The 5-HT5A receptor has been shown to be functional in a native expression system. Rodents have been shown to possess two functional 5-HT5 receptor subtypes, 5-HT5A and 5-HT5B, however while humans possess a gene coding for the 5-HT5B subtype, its co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mitochondrial Permeability Pore
The mitochondrial permeability transition pore (mPTP or MPTP; also referred to as PTP, mTP or MTP) is a protein that is formed in the inner membrane of the mitochondria under certain pathological conditions such as traumatic brain injury and stroke. Opening allows increase in the permeability of the mitochondrial membranes to molecules of less than 1500 Daltons in molecular weight. Induction of the permeability transition pore, mitochondrial membrane permeability transition (mPT or MPT), can lead to mitochondrial swelling and cell death through apoptosis or necrosis depending on the particular biological setting. Roles in pathology The MPTP was originally discovered by Haworth and Hunter in 1979 and has been found to be involved in neurodegeneration, hepatotoxicity from Reye-related agents, cardiac necrosis and nervous and muscular dystrophies among other deleterious events inducing cell damage and death. MPT is one of the major causes of cell death in a variety of conditi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Soviet Inventions
This timeline of Russian Innovation encompasses key events in the history of technology in Russia, from the Grand Duchy of Moscow up to the Russian Federation. The entries in this timeline fall into the following categories: * indigenous inventions, like airliners, AC transformers, radio receivers, television, artificial satellites, ICBMs * uniquely Russian products, objects and events, like Saint Basil's Cathedral, Matryoshka dolls, Russian vodka * products and objects with superlative characteristics, like the Tsar Bomba, the AK-47, and the Typhoon-class submarine * scientific and medical discoveries, like the periodic law, vitamins and stem cells This timeline includes scientific and medical discoveries, products and technologies introduced by various peoples of Russia and its predecessor states, regardless of ethnicity, and also lists inventions by naturalized immigrant citizens. Certain innovations achieved internationally may also appear in this timeline in cases wher ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Russian Drugs
Russian(s) refers to anything related to Russia, including: *Russians (, ''russkiye''), an ethnic group of the East Slavic peoples, primarily living in Russia and neighboring countries *Rossiyane (), Russian language term for all citizens and people of Russia, regardless of ethnicity *Russophone, Russian-speaking person (, ''russkogovoryashchy'', ''russkoyazychny'') *Russian language, the most widely spoken of the Slavic languages *Russian alphabet *Russian cuisine *Russian culture *Russian studies Russian may also refer to: *Russian dressing *''The Russians'', a book by Hedrick Smith *Russian (comics), fictional Marvel Comics supervillain from ''The Punisher'' series *Russian (solitaire), a card game * "Russians" (song), from the album ''The Dream of the Blue Turtles'' by Sting *"Russian", from the album ''Tubular Bells 2003'' by Mike Oldfield *"Russian", from the album '' '' by Caravan Palace *Nik Russian, the perpetrator of a con committed in 2002 *The South African name for a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyridines
Pyridine is a basic heterocyclic organic compound with the chemical formula . It is structurally related to benzene, with one methine group replaced by a nitrogen atom. It is a highly flammable, weakly alkaline, water-miscible liquid with a distinctive, unpleasant fish-like smell. Pyridine is colorless, but older or impure samples can appear yellow, due to the formation of extended, unsaturated polymeric chains, which show significant electrical conductivity. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Historically, pyridine was produced from coal tar. As of 2016, it is synthesized on the scale of about 20,000 tons per year worldwide. Properties Physical properties The molecular electric dipole moment is 2.2 debyes. Pyridine is diamagnetic and has a diamagnetic susceptibility of −48.7 × 10−6 cm3·mol−1. The standard enthalpy of formation is 100.2 kJ·mol−1 in the liquid phase ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
H1 Receptor Antagonists
H1 antagonists, also called H1 blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines; other agents may have antihistaminergic action but are not true antihistamines. In common use, the term "antihistamine" refers only to H1-antihistamines. Virtually all H1-antihistamines function as inverse agonists at the histamine H1-receptor, as opposed to neutral antagonists, as was previously believed. Medical uses H1-antihistamines are clinically used in the treatment of histamine-mediated allergic conditions. These indications may include:Rossi S (Ed.) (2004). ''Australian Medicines Handbook 2004''. Adelaide: Australian Medicines Handbook. * Allergic rhinitis * Allergic conjunctivitis * Allergic dermatological conditions (contact dermatitis) * Rhinorrhea (runny nose) * Urticaria * Angi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nootropics
Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic supplements or drugs and other substances that are claimed to improve cognitive function or to promote relaxation, particularly boosting mood, executive functions, attention, memory, creativity, or motivation in healthy individuals. The use of cognition-enhancing supplements by healthy individuals in the absence of a medical indication spans numerous controversial issues, including the ethics and fairness of their use, concerns over adverse effects, and the diversion of prescription drugs for non-medical uses. Nonetheless, the international sales of cognitive- or mood-enhancing supplements have continued to grow over time and in 2012 reached 0.69 billion. With sales supported by global health trends, the market is expected to reach US$33.85 billion by the year 2030, at a CAGR of 14.8%. While most nootropics are not regulated, there are othe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Idalopirdine
Idalopirdine (INN) (code names Lu AE58054,) is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia. As of October 2013 it is in phase III clinical trials. A phase III trial of two different daily doses of Lu AE58054 on top of 10 mg of donepezil for mild-to-moderate Alzheimer's failed to meet its primary endpoint Clinical endpoints or clinical outcomes are outcome measures referring to occurrence of disease, symptom, sign or laboratory abnormality constituting a target outcome in clinical research trials. The term may also refer to any disease or sign tha ... with either dose. Two further phase III trials failed too, the company confirmed in early 2017. See also * Cerlapirdine * Latrepirdine References External links Lundbeck expands its pipeline - initiating phase II clinical trials with a new compound for the treat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cerlapirdine
Cerlapirdine (USAN; SAM-531, WAY-262,531, PF-05212365) is a drug which was under development by Wyeth/Pfizer for the treatment of cognitive disorders associated with Alzheimer's disease and schizophrenia. In a phase II clinical trial it demonstrated a trend toward efficacy along with a good side effect profile and no incidence of serious adverse events, but no further development has occurred since 2011. It exerts its effects by acting as a selective 5-HT6 receptor antagonist. See also * Idalopirdine * Latrepirdine Latrepirdine ( INN, also known as dimebolin and sold as Dimebon) is an antihistamine drug which has been used clinically in Russia since 1983. Research was conducted in both Russia and western nations into potential applications as a neuroprotec ... References {{Serotonergics Dimethylamino compounds Abandoned drugs 1-Naphthyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
